in vitro PHARMACOLOGY 2011 CATALOG - Cerep

adykinin ❚
25
B 2
cellul ar
Ref. 1263
Ref. 1743
Q 3 weeks
Agonist effect
Antagonist effect
Source
human recombinant (CHO cells)
Measured product intracellular [Ca 2+ ]
Detection method fluorimetry
Agonist effect Control bradykinin (10 nM)
Reference bradykinin (EC 50 : 0.009 nM)
Antagonist effect Stimulant bradykinin (0.1 nM)
Reference HOE 140 (IC 50 : 85 nM)
Simpson, P.B. et al. (2000) Eur. J. Pharmacol., 392: 1-9.
Ca 2+ mobilization (% of control)
100
50
0
-13-12-11-10 -9 -8 -7 -6 -5 -4
log [agonist] (M)
bradykinin
desArg 9 -BK
kallidin
desArg 10 -KD
100
[Solvent] must be kept ≤ 0.1%
50
0
-12-11 -10 -9 -8 -7 -6 -5 -4
log [antagonist] (M)
HOE 140
NPC 567
LysdesArg 9 [Leu 8 ]-BK
bradyzide
Cerep
services
Receptors
[GPCRs]
B 2
tissue
Ref. 0623
Q 4 weeks
Source
human umbilical vein
Agonist bradykinin (pD 2 = 8.5)
Antagonist HOE 140 (pA 2 = 8.9)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Gobeil, F et al. (1996) Brit. J. Pharmacol., 118: 289-294.
-12 -11
-12 -11
-12 -11 -10 -9 -8 -7
-11 -10 -9 -8 -7 -6 -5 -4
-10 -9 -8 -7
-10 -9 -8 -7 -6 -5
-9 -8 -7 -6 -5
-10 -4
Ion
channels
Transporters
-11 -10 -9 -8 -7 -6 -5 -4
B 2
tissue
Ref. 0305
Q 4 weeks
Source
rabbit jugular vein
Agonist [Hyp 3 ,Tyr(Me) 8 ]-BK (pD 2 = 9.3)
Antagonist D-Arg[Hyp 3 ,D-Phe 7 ,Leu 8 ]-BK (pA 2 = 8.4)
Test concentrations 3 concentrations, n=2 (2 tissues)
for both activities
[Solvent] must be kept ≤ 0.1%
Rhaleb, N.-E et al. (1990) Brit. J. Pharmacol., 99: 445-448.
tension (% of max.)
100
50
0
-11 -10 -9 -8 -7
log [agonist] (M)
D-Arg[Hyp3,D-Phe7,
Leu8]-BK
none
10 nM
30 nM
100 nM
Kinases
Epigenetic &
DNA-related
enzymes
Other
enzymes
❚ calcitonin
Specialized
cellular
assays
CT (calcitonin) - agonist radioligand
Source
T47D cells (endogenous)
Ligand
[ 125 I]calcitonin (salmon) (0.05 nM)
Kd
0.045 nM
Non specific calcitonin (salmon) (0.5 µM)
binding
Reference calcitonin (salmon) (IC 50 : 0.5 nM)
Ref. 0728
Q 6 weeks
Kurokawa, M. et al. (1991) J. Endocrinol., 130: 321-326.
specific binding (% of control)
100
50
0
-11 -10 -9 -8 -7 -6 -5
log [drug] (M)
calcitonin
salmon
human
eel
porcine
Standard
profiles
Testing
conditions
CT (calcitonin)
cellul ar
Ref. 1964 Agonist effect
Ref. 1965 Antagonist effect
Q 3 weeks
Source
T47D cells (endogenous)
Measured product cAMP
Detection method HTRF
Agonist effect Control human calcitonin (1 µM)
Reference human calcitonin (EC 50 : 1.9 nM)
Antagonist effect Stimulant human calcitonin (30 nM)
Reference salmon calcitonin 8-32
(IC 50 : 25.8 nM)
Zimmermann, U. et al. (1997) J. Endocrinol., 155: 423-431.
cAMP modulation (% of control)
100
50
0
log [agonist] (M)
human calcitonin
salmon calcitonin
amylin
hCGRPα
100
-11 -10 -9 -8 -7 -6 -5 -11 -10 -9 -8 -7 -6 -5
[Solvent] must be kept ≤ 0.3%
50
0
log [antagonist] (M)
salmon calcitonin 8-32
CGRP 8-37
Ordering
information
Assay list
& index
-11 -10
-9 -8 -7 -6 -5 -4
-12 -11
-10 -9 -8 -7
-11 -10
-9 -8 -7 -6 -5 -4